AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML)
Zarrinkar, Patrick P., Gunawardane, Ruwanthi N., Cramer, Merryl D., Gardner, Michael F., Brigham, Daniel, Belli, Barbara, Karaman, Mazen W., Pratz, Keith W., Pallares, Gabriel, Chao, Qi, Sprankle, Kelly G., Patel, Hitesh K., Levis, Mark, Armstrong, Robert C., James, Joyce, Bhagwat, Shripad S.
Published in Blood (01.10.2009)
Published in Blood (01.10.2009)
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Identification of N-(5-tert-Butyl-isoxazol-3-yl)-N′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea Dihydrochloride (AC220), a Uniquely Potent, Selective, and Efficacious FMS-Like Tyrosine Kinase-3 (FLT3) Inhibitor
Chao, Qi, Sprankle, Kelly G, Grotzfeld, Robert M, Lai, Andiliy G, Carter, Todd A, Velasco, Anne Marie, Gunawardane, Ruwanthi N, Cramer, Merryl D, Gardner, Michael F, James, Joyce, Zarrinkar, Patrick P, Patel, Hitesh K, Bhagwat, Shripad S
Published in Journal of medicinal chemistry (10.12.2009)
Published in Journal of medicinal chemistry (10.12.2009)
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Identification of 1-(3-(6,7-Dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea Hydrochloride (CEP-32496), a Highly Potent and Orally Efficacious Inhibitor of V-RAF Murine Sarcoma Viral Oncogene Homologue B1 (BRAF) V600E
Rowbottom, Martin W, Faraoni, Raffaella, Chao, Qi, Campbell, Brian T, Lai, Andiliy G, Setti, Eduardo, Ezawa, Maiko, Sprankle, Kelly G, Abraham, Sunny, Tran, Lan, Struss, Brian, Gibney, Michael, Armstrong, Robert C, Gunawardane, Ruwanthi N, Nepomuceno, Ronald R, Valenta, Ianina, Hua, Helen, Gardner, Michael F, Cramer, Merryl D, Gitnick, Dana, Insko, Darren E, Apuy, Julius L, Jones-Bolin, Susan, Ghose, Arup K, Herbertz, Torsten, Ator, Mark A, Dorsey, Bruce D, Ruggeri, Bruce, Williams, Michael, Bhagwat, Shripad, James, Joyce, Holladay, Mark W
Published in Journal of medicinal chemistry (09.02.2012)
Published in Journal of medicinal chemistry (09.02.2012)
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CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity
James, Joyce, Ruggeri, Bruce, Armstrong, Robert C, Rowbottom, Martin W, Jones-Bolin, Susan, Gunawardane, Ruwanthi N, Dobrzanski, Pawel, Gardner, Michael F, Zhao, Hugh, Cramer, Merryl D, Hunter, Kathryn, Nepomuceno, Ronald R, Cheng, Mangeng, Gitnick, Dana, Yazdanian, Mehran, Insko, Darren E, Ator, Mark A, Apuy, Julius L, Faraoni, Raffaella, Dorsey, Bruce D, Williams, Michael, Bhagwat, Shripad S, Holladay, Mark W
Published in Molecular cancer therapeutics (01.04.2012)
Published in Molecular cancer therapeutics (01.04.2012)
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Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors
Abraham, Sunny, Hadd, Michael J., Tran, Lan, Vickers, Troy, Sindac, Janice, Milanov, Zdravko V., Holladay, Mark W., Bhagwat, Shripad S., Hua, Helen, Ford Pulido, Julia M., Cramer, Merryl D., Gitnick, Dana, James, Joyce, Dao, Alan, Belli, Barbara, Armstrong, Robert C., Treiber, Daniel K., Liu, Gang
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
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Journal Article
4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors
Holladay, Mark W., Campbell, Brian T., Rowbottom, Martin W., Chao, Qi, Sprankle, Kelly G., Lai, Andiliy G., Abraham, Sunny, Setti, Eduardo, Faraoni, Raffaella, Tran, Lan, Armstrong, Robert C., Gunawardane, Ruwanthi N., Gardner, Michael F., Cramer, Merryl D., Gitnick, Dana, Ator, Mark A., Dorsey, Bruce D., Ruggeri, Bruce R., Williams, Michael, Bhagwat, Shripad S., James, Joyce
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
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METABOLISM AND DISPOSITION OF A POTENT GROUP II METABOTROPIC GLUTAMATE RECEPTOR AGONIST, IN RATS, DOGS, AND MONKEYS
JAMES, Joyce K, NAKAMURA, Masato, NAKAZATO, Atsuro, ZHANG, Kanyin E, CRAMER, Merryl, BRUNNER, Janice, COOK, Jacquelynn, CHEN, Weichao G
Published in Drug metabolism and disposition (01.09.2005)
Published in Drug metabolism and disposition (01.09.2005)
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CEP-32496: A Novel Orally Active BRAFV600E Inhibitor with Selective Cellular and In Vivo Antitumor Activity
James, Joyce, Ruggeri, Bruce, Armstrong, Robert C., Rowbottom, Martin W., Jones-Bolin, Susan, Gunawardane, Ruwanthi N., Dobrzanski, Pawel, Gardner, Michael F., Zhao, Hugh, Cramer, Merryl D., Hunter, Kathryn, Nepomuceno, Ronald R., Cheng, Mangeng, Gitnick, Dana, Yazdanian, Mehran, Insko, Darren E., Ator, Mark A., Apuy, Julius L., Faraoni, Raffaella, Dorsey, Bruce D., Williams, Michael, Bhagwat, Shripad S., Holladay, Mark W.
Published in Molecular cancer therapeutics (01.04.2012)
Published in Molecular cancer therapeutics (01.04.2012)
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Biphenyl-indanones: Allosteric potentiators of the metabotropic glutamate subtype 2 receptor
Bonnefous, Céline, Vernier, Jean-Michel, Hutchinson, John H., Gardner, Michael F., Cramer, Merryl, James, Joyce K., Rowe, Blake A., Daggett, Lorrie P., Schaffhauser, Hervé, Kamenecka, Theodore M.
Published in Bioorganic & medicinal chemistry letters (01.10.2005)
Published in Bioorganic & medicinal chemistry letters (01.10.2005)
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Journal Article
4-Quinazolinyloxy-diaryl ureas as novel BRAF super(V600E inhibitors)
Holladay, Mark W, Campbell, Brian T, Rowbottom, Martin W, Chao, Qi, Sprankle, Kelly G, Lai, Andiliy G, Abraham, Sunny, Setti, Eduardo, Faraoni, Raffaella, Tran, Lan, Armstrong, Robert C, Gunawardane, Ruwanthi N, Gardner, Michael F, Cramer, Merryl D, Gitnick, Dana, Ator, Mark A, Dorsey, Bruce D, Ruggeri, Bruce R, Williams, Michael, Bhagwat, Shripad S, James, Joyce
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
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Journal Article
In vitro metabolic studies on the selective metabotropic glutamate receptor sub-type 5 (mGluR5) antagonist 3-[(2-methyl-1,3-thiazol-4-yl) ethynyl]-pyridine (MTEP)
GREEN, Mitchell D, XIAOQING YANG, CRAMER, Merryl, KING, Christopher D
Published in Neuroscience letters (2005)
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Published in Neuroscience letters (2005)
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5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3′-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity
Roppe, Jeffrey R, Wang, Bowei, Huang, Dehua, Tehrani, Lida, Kamenecka, Theodore, Schweiger, Edwin J, Anderson, Jeffery J, Brodkin, Jesse, Jiang, Xiaohui, Cramer, Merryl, Chung, Janice, Reyes-Manalo, Grace, Munoz, Benito, Cosford, Nicholas D.P
Published in Bioorganic & medicinal chemistry letters (02.08.2004)
Published in Bioorganic & medicinal chemistry letters (02.08.2004)
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Journal Article
3-[3-Fluoro-5-(5-pyridin-2-yl-2 H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist
Poon, Steve F., Eastman, Brian W., Chapman, Deborah F., Chung, Janice, Cramer, Merryl, Holtz, Gregory, Cosford, Nicholas D.P., Smith, Nicholas D.
Published in Bioorganic & medicinal chemistry letters (15.11.2004)
Published in Bioorganic & medicinal chemistry letters (15.11.2004)
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Journal Article
2-{2-[3-(Pyridin-3-yloxy)phenyl]-2 H-tetrazol-5-yl}pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist
Huang, Dehua, Poon, Steve F., Chapman, Deborah F., Chung, Janice, Cramer, Merryl, Reger, Thomas S., Roppe, Jeffrey R., Tehrani, Lida, Cosford, Nicholas D.P., Smith, Nicholas D.
Published in Bioorganic & medicinal chemistry letters (15.11.2004)
Published in Bioorganic & medicinal chemistry letters (15.11.2004)
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Journal Article
In vitro metabolic studies on the selective metabotropic glutamate receptor sub-type 5 (mGluR5) antagonist 3-[(2-methyl-1,3-thiazol-4-yl) ethynyl]-pyridine (MTEP)
Green, Mitchell D., Yang, Xiaoqing, Cramer, Merryl, King, Christopher D.
Published in Neuroscience letters (02.01.2006)
Published in Neuroscience letters (02.01.2006)
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Journal Article
Synthesis and biological evaluation of 6-aryl-6H-pyrrolo[3,4-d]pyridazine derivatives: high-affinity ligands to the α2δ subunit of voltage gated calcium channels
STEARNS, Brian A, ANKER, Naomi, SABLAD, Marciano, SANTINI, Angelina, SCHAFFHAUSER, Herve, URBAN, Mark O, MUNOZ, Benito, ARRUDA, Jeannie M, CAMPBELL, Brian T, CHIXU CHEN, CRAMER, Merryl, TAO HU, XIAOHUI JIANG, PARK, Kenneth, KUN KUN REN
Published in Bioorganic & medicinal chemistry letters (08.03.2004)
Published in Bioorganic & medicinal chemistry letters (08.03.2004)
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3-[Substituted]-5-(5-pyridin-2-yl-2 H-tetrazol-2-yl)benzonitriles: Identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists
Tehrani, Lida R., Smith, Nicholas D., Huang, Dehua, Poon, Steve F., Roppe, Jeffrey R., Seiders, Thomas Jon, Chapman, Deborah F., Chung, Janice, Cramer, Merryl, Cosford, Nicholas D.P.
Published in Bioorganic & medicinal chemistry letters (15.11.2005)
Published in Bioorganic & medicinal chemistry letters (15.11.2005)
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Journal Article
Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity
Smith, Nicholas D., Poon, Steve F., Huang, Dehua, Green, Mitchell, King, Christopher, Tehrani, Lida, Roppe, Jeffrey R., Chung, Janice, Chapman, Deborah P., Cramer, Merryl, Cosford, Nicholas D.P.
Published in Bioorganic & medicinal chemistry letters (15.11.2004)
Published in Bioorganic & medicinal chemistry letters (15.11.2004)
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Journal Article
Water soluble prodrug of a COX-2 selective inhibitor suitable for intravenous administration in models of cerebral ischemia
Smith, Nicholas D., Reger, Thomas S., Payne, Joseph, Zunic, Jasmine, Lorrain, Dan, Correa, Lucie, Stock, Nicholas, Cramer, Merryl, Chen, Weichao, Yang, Jennifer, Prasit, Peppi, Munoz, Benito
Published in Bioorganic & medicinal chemistry letters (01.07.2005)
Published in Bioorganic & medicinal chemistry letters (01.07.2005)
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Journal Article
Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists
Chua, Peter C., Nagasawa, Johnny Y., Bleicher, Leo S., Munoz, Benito, Schweiger, Edwin J., Tehrani, Lida, Anderson, Jeffrey J., Cramer, Merryl, Chung, Janice, Green, Mitchell D., King, Chris D., Reyes-Manalo, Grace, Cosford, Nicholas D.P.
Published in Bioorganic & medicinal chemistry letters (15.10.2005)
Published in Bioorganic & medicinal chemistry letters (15.10.2005)
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